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Tofisopam

Tofisopam structure

CAS No:
22345-47-7
Formula:
C22H26N2O4
Chemical Name:
Tofisopam
Synonyms:
5H-2,3-Benzodiazepine,1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-;1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine;Tofisopam;Grandaxin;EGYT 341;7,8-Dimethoxy-1-(3,4-dimethoxyphenyl)-5-ethyl-4-methyl-5H-2,3-benzodiazepine;Seriel;1-(3,4-Dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine;Nodeprine;1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-benzo[d][1,2]diazepine;87555-18-8
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Solid

Tofisopam is an organic molecular entity.|Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine drug which is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Although Tofisopam is not approved for sale in North America, it is approved for use in various countries worldwide, including parts of Europe. The D-enantiomer ([dextofisopam]) is currently in phase II trials in the U.S. for the treatment of irritable bowel syndrome.

Tofisopam Basic Attributes

Molecular Weight：

382.45300

Exact Mass：

382.45

EC Number：

244-922-3

DSSTox ID：

DTXSID3023681

ATC Code：

N - Nervous system

Characteristics

PSA：

61.64000

XLogP3：

3.31270

Appearance：

white solid

Density：

1.15g/cm3

Melting Point：

156.5 °C

Boiling Point：

479ºC at 760 mmHg

Flash Point：

195.2ºC

Refractive Index：

1.558

Vapor Pressure：

7.13E-09mmHg at 25°C

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

UN 3077

wgk germany：

hazard class code：

R22; R50

safety instructions：

60-61

RTECS Number：

DE9540000

Marks：

Xn; N

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, P391, and P501|Aggregated GHS information provided by 40 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity Summary：

The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma (Grade I or Grade II) following very large ingestions. Oral, rat LD50 is 825 mg/kg.

Drug Information

Drug Indication：

For the treatment of anxiety and alcohol withdrawal.

Pharmacology：

Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. It enhances the anticonvulsant activity of 1,4-benzodiazepines like diazepam but not sodium valproate, carbamazepine, phenobarbital, or phenytoin.

MeSH：

Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems. (See all compounds classified as Antidepressive Agents.)

Metabolism/Metabolites：

Hepatic.

Biological Half-Life：

6-8 hours

Mechanism of Action：

Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study (Rundfeldt C. et al.) has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with highest affinity to PDE-4A1 (0.42 μM) followed by PDE-10A1 (0.92 μM), PDE-3 (1.98 μM) and PDE-2A3 (2.11 μM).

MeSH Entry Terms：

1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine

Computed Properties

Molecular Weight:382.5
XLogP3:3.2
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:6
Exact Mass:382.18925731
Monoisotopic Mass:382.18925731
Topological Polar Surface Area:61.6
Heavy Atom Count:28
Complexity:579
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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CAS No.: 22345-47-7

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